Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity

• Published in: Acta pharmaceutica (Zagreb, Croatia) Vol. 73; no. 3; pp. 457 - 473
• Main Authors: Solís-Cruz, Guadalupe Y., Alvarez-Roman, Rocío, Rivas-Galindo, Verónica M., Galindo-Rodríguez, Sergio Arturo, Silva-Mares, David A., Marino-Martínez, Iván A., Escobar-Saucedo, Magdalena, Pérez-López, Luis A.
• Format: Journal Article
• Language: English
• Published: Zagreb Sciendo 01.09.2023; De Gruyter Poland
• Subjects: antiviral; Controlled release; Dichloromethane; Diterpenes; herpes simplex virus; Nanoparticles; Optimization; Polydispersity; polymeric nanoparticles; riolozatrione; Sustained release; Zeta potential
• ISSN: 1846-9558; 1330-0075; 1846-9558
• DOI: 10.2478/acph-2023-0028

Riolozatrione (RZ) is a diterpenoid compound isolated from a dichloromethane extract of the root. This compound has been shown to possess moderate antiherpetic activity . However, because of the poor solubility of this compound in aqueous vehicles, generating a stable formulation for potential use in the treatment of infection is challenging. The aim of this work was to optimize and physio-chemically characterize Eudragit L100-55-based polymeric nanoparticles (NPs) loaded with RZ (NPR) for antiherpetic application. The NPs formulation was initially optimized using the dichloromethane extract of , the major component of which was RZ. The optimized NPR formulation was stable, with a size of 263 nm, polydispersity index < 0.2, the zeta potential of –37 mV, and RZ encapsulation efficiency of 89 %. The NPR showed sustained release of RZ for 48 h with release percentages of 95 and 97 % at neutral and slightly acidic pH, respectively. Regarding antiherpetic activity, the optimized NPR showed a selectivity index for HSV-1 of ≈16 and for HSV-2 of 13.